Design, synthesis and structure-activity relationships of novel strychnine-insensitive glycine receptor ligands

Bioorg Med Chem Lett. 1999 May 17;9(10):1409-14. doi: 10.1016/s0960-894x(99)00194-8.

Abstract

The in vitro activities of 3-hydroxy-imidazolidin-4-one derivatives demonstrated very restricted structure-activity relationships at the strychnine-insensitive glycine site of the NMDA receptor. The most active compound (3a) was completely unsubstituted and exhibited affinity and efficacy similar to that of D-cycloserine, the prototypical partial agonist at this site.

MeSH terms

  • Drug Design*
  • Glycine / metabolism*
  • Imidazoles / chemical synthesis
  • Imidazoles / chemistry*
  • Imidazoles / pharmacology*
  • Ligands
  • Receptors, N-Methyl-D-Aspartate / chemistry
  • Receptors, N-Methyl-D-Aspartate / metabolism*
  • Structure-Activity Relationship
  • Strychnine / pharmacology*

Substances

  • 3-hydroxyimidazolidin-4-one
  • Imidazoles
  • Ligands
  • Receptors, N-Methyl-D-Aspartate
  • Strychnine
  • Glycine